product name AZ5104
Description: AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Compare to AZD9291, AZ5104 has higher potency in mutant EGFR cell lines ex19del (2 nmol/L in PC-9), T790M (2 nmol/L in H1975), and wild-type EGFR (33 nmol/L in LOVO) cell lines. In a phenotypic assay, AZ5104 showed a greater potency across cell lines in a phenotypic assay.
References: Cancer Discov. 2014 Sep;4(9):1046-61.
485.58
Formula
C27H31N7O2
CAS No.
1421373-98-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 97 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 23 mg/mL (47.4 mM)
Solubility (In vivo)
1% Tween 80: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19416329
| In Vitro |
In vitro activity: AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. Kinase Assay: Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase. Cell Assay: |
|---|---|
| In Vivo | In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. |
| Animal model | Mice bearing C/L858R and C/L+T tumors |
| Formulation & Dosage | Dissolved in 1% Polysorbate 80; 5 mg/kg; Oral gavage |
| References | Cancer Discov. 2014 Sep;4(9):1046-61. |
